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- W2916524159 endingPage "82" @default.
- W2916524159 startingPage "82" @default.
- W2916524159 abstract "Phosphatidylinositol 3-kinases (PI3Ks) are important therapeutic targets for the treatment of cancer, thrombosis, and inflammatory and immune diseases. The four highly homologous Class I isoforms, PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ have unique, non-redundant physiological roles and as such, isoform selectivity has been a key consideration driving inhibitor design and development. In this review, we discuss the structural biology of PI3Ks and how our growing knowledge of structure has influenced the medicinal chemistry of PI3K inhibitors. We present an analysis of the available structure-selectivity-activity relationship data to highlight key insights into how the various regions of the PI3K binding site influence isoform selectivity. The picture that emerges is one that is far from simple and emphasizes the complex nature of protein-inhibitor binding, involving protein flexibility, energetics, water networks and interactions with non-conserved residues." @default.
- W2916524159 created "2019-03-02" @default.
- W2916524159 creator A5029031647 @default.
- W2916524159 creator A5032907078 @default.
- W2916524159 creator A5077581858 @default.
- W2916524159 date "2019-02-26" @default.
- W2916524159 modified "2023-10-16" @default.
- W2916524159 title "Structural Determinants of Isoform Selectivity in PI3K Inhibitors" @default.
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